4lxm

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m (Protected "4lxm" [edit=sysop:move=sysop])
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'''Unreleased structure'''
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{{STRUCTURE_4lxm| PDB=4lxm | SCENE= }}
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===Crystal Structure of Human Beta Secretase in Complex with compound 12a===
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{{ABSTRACT_PUBMED_22380629}}
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The entry 4lxm is ON HOLD
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==Function==
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[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>
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Authors: Rondeau, J.M., Bourgier, E.
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==About this Structure==
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[[4lxm]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Ochroconis_lascauxensis Ochroconis lascauxensis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LXM OCA].
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Description: Crystal Structure of Human Beta Secretase in Complex with compound 12a
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==Reference==
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<ref group="xtra">PMID:022380629</ref><references group="xtra"/><references/>
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[[Category: Memapsin 2]]
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[[Category: Ochroconis lascauxensis]]
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[[Category: Bourgier, E.]]
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[[Category: Rondeau, J M.]]
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[[Category: Aspartyl protease]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Membrane]]
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[[Category: Structure-based drug design]]

Revision as of 07:30, 28 August 2013

Template:STRUCTURE 4lxm

Contents

Crystal Structure of Human Beta Secretase in Complex with compound 12a

Template:ABSTRACT PUBMED 22380629

Function

[BACE1_HUMAN] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.[1] [2]

About this Structure

4lxm is a 3 chain structure with sequence from Ochroconis lascauxensis. Full crystallographic information is available from OCA.

Reference

  • Rueeger H, Lueoend R, Rogel O, Rondeau JM, Mobitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U. Discovery of cyclic sulfone hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid beta-peptides. J Med Chem. 2012 Apr 12;55(7):3364-86. Epub 2012 Mar 21. PMID:22380629 doi:10.1021/jm300069y
  1. ↑ Lin X, Koelsch G, Wu S, Downs D, Dashti A, Tang J. Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1456-60. PMID:10677483
  2. ↑ Okada H, Zhang W, Peterhoff C, Hwang JC, Nixon RA, Ryu SH, Kim TW. Proteomic identification of sorting nexin 6 as a negative regulator of BACE1-mediated APP processing. FASEB J. 2010 Aug;24(8):2783-94. doi: 10.1096/fj.09-146357. Epub 2010 Mar 30. PMID:20354142 doi:10.1096/fj.09-146357

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